3-(Difluoromethoxy)pyridine-2-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-(Difluoromethoxy)pyridine-2-carboxamide
• 英文别名: 3-(difluoromethoxy)pyridine-2-carboxamide
• 化学式: C₇H₆F₂N₂O₂
• 分子量: 188.13
• InChiKey: QIWBLKMCIUSZNP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  65.2
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] BACE1 INHIBITORS<br/>[FR] INHIBITEURS DE BACE1
  申请人：HOFFMANN LA ROCHE

  公开号：WO2016055496A1

  公开（公告）日：2016-04-14

  The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

  本发明提供了一种具有BACE1抑制活性的I式化合物，其制备方法，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗例如阿尔茨海默病等疾病中是有用的。
• [EN] 2-AMINO-6-METHYL-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]THIAZIN-8a(8H)-YL-1,3-THIAZOL-4-YL AMIDES<br/>[FR] AMIDES 2-AMINO-6-MÉTHYL-4,4A,5,6-TÉTRAHYDROPYRANO[3,4-D][1,3]THIAZIN-8A(8H)-YL-1,3-THIAZOL-4-YLE
  申请人：PFIZER

  公开号：WO2015155626A1

  公开（公告）日：2015-10-15

  The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula (I), and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  本发明涉及所披露的化合物、互变异构体和药学上可接受的盐，其中所述化合物具有式(I)的结构，变量R1如规范中所定义。还披露了相应的药物组合物、治疗方法、合成方法和中间体。
• [EN] TETRAHYDROPYRANO[3,4-D][1,3]OXAZIN DERIVATIVES AND THEIR USE AS BACE INHIBITORS<br/>[FR] DÉRIVÉS DE TÉTRAHYDROPYRANO[3,4-D] [1,3]OXAZINE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE BACE
  申请人：PFIZER

  公开号：WO2017051303A1

  公开（公告）日：2017-03-30

  The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula (I), wherein the variables R1, R2, R3, R4 and X are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  本发明涉及所披露的化合物、互变异构体和该化合物的药学上可接受的盐，其中该化合物具有公式（I）的结构，其中变量R1、R2、R3、R4和X如规范中定义。还披露了相应的药物组合物、治疗方法、合成方法和中间体。
• [EN] N-[2-(3-AMINO-2,5-DIMETHYL-1,1-DIOXIDO-5,6-DIHYDRO-2H-1,2,4-THIADIAZIN-5-YL)-1,3-THIAZOL-4-YL] AMIDES USEFUL AS BACE INHIBITORS<br/>[FR] N-[2-(3-AMINO-2,5-DIMÉTHYL-1,1-DIOXIDO-5,6-DIHYDRO-2H-1,2,4-THIADIAZIN-5-YL)-1,3-THIAZOL-4-YL] AMIDES UTILES COMME INHIBITEURS DE BACE
  申请人：PFIZER

  公开号：WO2017051294A1

  公开（公告）日：2017-03-30

  The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1, R2 and R3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  本发明涉及所披露的化合物、互变异构体和该化合物的药用可接受盐，其中该化合物具有如下式I的结构，其中变量R1、R2和R3如规范中所定义。同时也披露了相应的药用组合物、治疗方法、合成方法和中间体。
• N-[2-(2-amino-6,6-disubstituted-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-YL)-1,3-thiazol-4-YL] amides
  申请人：Pfizer Inc.

  公开号：US10112958B2

  公开（公告）日：2018-10-30

  The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1, R2 and R3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  本发明涉及所公开的化合物、同系物和药学上可接受的盐，其中化合物具有式 I 的结构、 变量 R1、R2 和 R3 如说明书中所定义。还公开了相应的药物组合物、治疗方法、合成方法和中间体。